Delineating the role of cooperativity in the design of potent PROTACs for BTK

Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon

(2018) Afua A. Akuffo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

BTKC481S-Mediated Resistance to Ibrutinib in Chronic Lymphocytic Leukemia

(2017) Jennifer A. Woyach et al.   JOURNAL OF CLINICAL ONCOLOGY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase

(2017) Jian An et al.   Nature Communications

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The structure and regulation of Cullin 2 based E3 ubiquitin ligases and their biological functions

(2016) Weijia Cai et al.   Cell Division

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

(2015) Ashton C. Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Ibrutinib in B-cell Lymphomas

(2014) Kami Maddocks et al.   CURRENT TREATMENT OPTIONS IN ONCOLOGY

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

(2014) Bryan R Lanning et al.   Nature Chemical Biology

NuRD–ZNF827 recruitment to telomeres creates a molecular scaffold for homologous recombination

(2014) Dimitri Conomos et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Building and remodelling Cullin-RING E3 ubiquitin ligases

(2013) John R Lydeard et al.   EMBO REPORTS

Selective Inhibition of BTK Prevents Murine Lupus and Antibody-Mediated Glomerulonephritis

(2013) A. L. Rankin et al.   JOURNAL OF IMMUNOLOGY

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

(2013) Eugene F. Douglass et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting BTK with Ibrutinib in Relapsed or Refractory Mantle-Cell Lymphoma

(2013) Michael L. Wang et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

Inhibitor of Apoptosis (IAP) Proteins-Modulators of Cell Death and Inflammation

(2013) J. Silke et al.   Cold Spring Harbor Perspectives in Biology

Bruton’s Tyrosine Kinase (BTK) Inhibitors in Clinical Trials

(2013) Jan A. Burger   Current Hematologic Malignancy Reports

X-linked inhibitor of apoptosis protein mediates neddylation by itself but does not function as a NEDD8-E3 ligase for caspase-7

(2012) Taiki Nagano et al.   FEBS LETTERS

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Structure-based prediction of protein–protein interactions on a genome-wide scale

(2012) Qiangfeng Cliff Zhang et al.   NATURE

Development of target protein-selective degradation inducer for protein knockdown

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy

(2011) Yosuke Demizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Molecular Basis of CRL4DDB2/CSA Ubiquitin Ligase Architecture, Targeting, and Activation

(2011) Eric S. Fischer et al.   CELL

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein

(2011) Keiichiro Okuhira et al.   FEBS LETTERS

Structural assembly of cullin-RING ubiquitin ligase complexes

(2010) Erik S Zimmerman et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

(2009) Abdalla J. Mohamed et al.   IMMUNOLOGICAL REVIEWS

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structural Basis of UV DNA-Damage Recognition by the DDB1–DDB2 Complex

(2008) Andrea Scrima et al.   CELL

Genome-Wide and Functional Annotation of Human E3 Ubiquitin Ligases Identifies MULAN, a Mitochondrial E3 that Regulates the Organelle's Dynamics and Signaling

(2008) Wei Li et al.   PLoS One